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Catalog No. Product Name Information Product Use Citations Product Validations
S0278 SU5614 SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis.
Adv Sci (Weinh), 2021, e2101848
S0377 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
S0504 SU14813 SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity.
Adv Sci (Weinh), 2021, e2101848
S1005 Axitinib (AG 013736) Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
J Ethnopharmacol, 2022, 288:114969
J Clin Invest, 2021, 131(8)139434
Theranostics, 2021, 11(10):4975-4991
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Hum Mol Genet, 2021, ddab009
Sci Rep, 2021, 11(1):9362
Sci Rep, 2021, 11(1):23302
S1018 Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Immunol, 2022, ji2100400
Nat Immunol, 2021, 10.1038/s41590-021-00948-8
S1026 Imatinib (STI571) Mesylate Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cell Rep, 2021, 37(1):109788
S1032 Motesanib Diphosphate (AMG-706) Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
Drug Metab Dispos, 2021, 49(1):53-61
Cell Stem Cell, 2019, 25(1):69-86
J Virol, 2019, 10.1128/JVI.01791-19
S1035 Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(14)3635
J Clin Endocrinol Metab, 2021, dgab020
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cell Death Dis, 2022, 13(1):35
Cancer Cell, 2021, S1535-6108(21)00659-0
Leukemia, 2021, 10.1038/s41375-021-01308-z
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, 8(2):2001596
Adv Sci (Weinh), 2021, 8(2):2001596
S1064 Masitinib (AB1010) Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Drug Metab Dispos, 2021, 49(1):53-61
Res Vet Sci, 2021, 138:178-187
S1111 Foretinib (GSK1363089) Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Cancers (Basel), 2021, 13(3)E372
Cancers (Basel), 2021, 13(19)5012
Mol Carcinog, 2021, 60(7):481-496
S1164 Lenvatinib (E7080) Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.
Nature, 2021, 595(7869):730-734
Cancer Cell, 2021, S1535-6108(21)00659-0
Hepatology, 2021, 10.1002/hep.31921
S1178 Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, e2103360
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
S1207 Tivozanib (AV-951) Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cell Syst, 2020, 10(3):240-253
S1220 OSI-930 OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.
Cell Rep, 2019, 28(9):2331-2344
Nat Biomed Eng, 2018, 2(8):578-588
Mol Syst Biol, 2015, 11(1):789
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
mBio, 2021, 12(6):e0322821
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1363 Ki8751 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
Front Oncol, 2021, 11:650052
J Clin Med, 2020, 9(3)
Front Pharmacol, 2020, 11:572624
S2070 ISCK03 ISCK03 (N-(4-imidazol-1-yl phenyl)sulfonamide) is a cell-permeable inhibitor of stem-cell factor (SCF)/c-kit signaling.ISCK03 inhibits SCF-induced c-c-kit phosphorylation and downstream ERK phosphorylation.
S2231 Telatinib Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.
Cell Stem Cell, 2019, 24(4):654-669
Clin Cancer Res, 2018, 24(11):2678-2687
Biochem Pharmacol, 2014, 89(1):52-61
S2475 Imatinib (STI571) Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Cell Host Microbe, 2021, 29(6):941-958.e10
Nat Commun, 2021, 12(1):51
Clin Cancer Res, 2021, 27(9):2533-2548
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cancer Res, 2021, canres.1222.2021
Cancers (Basel), 2021, 13(14)3635
Radiother Oncol, 2021, 157:175-181
S4001 Cabozantinib malate (XL184) Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(14)3635
S4947New Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Int J Mol Sci, 2021, 22(21)11770
S5077 Regorafenib (BAY-734506) Monohydrate Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Neoplasia, 2021, 23(3):304-325
S5240 Lenvatinib (E7080) Mesylate Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.
J Immunother Cancer, 2021, 9(6)e002305
Cancer Lett, 2021, 519:46-62
Cancers (Basel), 2021, 13(11)2539
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Front Oncol, 2021, 11:739139
Biochem Biophys Res Commun, 2021, 586:177-184
Cells, 2020, 9(6):E1452
S6662 AST-487 (NVP-AST487) AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.
Nat Commun, 2020, 21;11(1):1924
S7003 AZD2932 AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
Cancer Res, 2020, canres.1992.2020
Molecules, 2020, 8;25(9) pii: E2220
Development, 2016, 143(23):4394-4404
S7688 Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258, CHIR258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S7781 Sunitinib (SU11248) Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Adv Sci (Weinh), 2021, e2100881
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Blood Cancer J, 2021, 11(3):57
S7782 Dasatinib Monohydrate Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Nat Commun, 2021, 12(1):3705
Nucleic Acids Res, 2021, gkab538
S7818 Pexidartinib (PLX3397) Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.
Cell Death Dis, 2022, 13(1):33
Sci Transl Med, 2021, 13(598)eabd4550
J Exp Med, 2021, 218(8)e20210542
S8015 Agerafenib (RXDX-105) Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Mol Pharmacol, 2021, 99(6):435-447
Dis Model Mech, 2020, dmm.047779
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
J Cardiovasc Dev Dis, 2021, 8(3)28
Mol Med Rep, 2021, 23(4):1
CellPress, 2021, None
S8401 Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
Oncoimmunology, 2022, 11(1):2021619
Nature, 2021, 10.1038/s41586-020-03085-8
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
S8553 Avapritinib (BLU-285) Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
JCI Insight, 2020, 143474
J Pers Med, 2020, 10(4)E234
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
S8721 PDGFR inhibitor 1 PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.
S8757 Ripretinib (DCC-2618) DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.
Cancers (Basel), 2021, 13(15)3699
J Pers Med, 2020, 10(4)E234
Expert Opin Pharmacother, 2019, 20(13):1539-1550
S8780 AZD3229 AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
Front Immunol, 2020, 11:564133
Cell Signal, 2014, 26(1):149-61
S0278 SU5614 SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis.
Adv Sci (Weinh), 2021, e2101848
S0377 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
S0504 SU14813 SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity.
Adv Sci (Weinh), 2021, e2101848
S1005 Axitinib (AG 013736) Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
J Ethnopharmacol, 2022, 288:114969
J Clin Invest, 2021, 131(8)139434
Theranostics, 2021, 11(10):4975-4991
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Hum Mol Genet, 2021, ddab009
Sci Rep, 2021, 11(1):9362
Sci Rep, 2021, 11(1):23302
S1018 Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Immunol, 2022, ji2100400
Nat Immunol, 2021, 10.1038/s41590-021-00948-8
S1026 Imatinib (STI571) Mesylate Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cell Rep, 2021, 37(1):109788
S1032 Motesanib Diphosphate (AMG-706) Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
Drug Metab Dispos, 2021, 49(1):53-61
Cell Stem Cell, 2019, 25(1):69-86
J Virol, 2019, 10.1128/JVI.01791-19
S1035 Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(14)3635
J Clin Endocrinol Metab, 2021, dgab020
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cell Death Dis, 2022, 13(1):35
Cancer Cell, 2021, S1535-6108(21)00659-0
Leukemia, 2021, 10.1038/s41375-021-01308-z
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, 8(2):2001596
Adv Sci (Weinh), 2021, 8(2):2001596
S1064 Masitinib (AB1010) Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Drug Metab Dispos, 2021, 49(1):53-61
Res Vet Sci, 2021, 138:178-187
S1111 Foretinib (GSK1363089) Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Cancers (Basel), 2021, 13(3)E372
Cancers (Basel), 2021, 13(19)5012
Mol Carcinog, 2021, 60(7):481-496
S1164 Lenvatinib (E7080) Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.
Nature, 2021, 595(7869):730-734
Cancer Cell, 2021, S1535-6108(21)00659-0
Hepatology, 2021, 10.1002/hep.31921
S1178 Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, e2103360
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
S1207 Tivozanib (AV-951) Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cell Syst, 2020, 10(3):240-253
S1220 OSI-930 OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.
Cell Rep, 2019, 28(9):2331-2344
Nat Biomed Eng, 2018, 2(8):578-588
Mol Syst Biol, 2015, 11(1):789
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
mBio, 2021, 12(6):e0322821
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1363 Ki8751 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
Front Oncol, 2021, 11:650052
J Clin Med, 2020, 9(3)
Front Pharmacol, 2020, 11:572624
S2070 ISCK03 ISCK03 (N-(4-imidazol-1-yl phenyl)sulfonamide) is a cell-permeable inhibitor of stem-cell factor (SCF)/c-kit signaling.ISCK03 inhibits SCF-induced c-c-kit phosphorylation and downstream ERK phosphorylation.
S2231 Telatinib Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.
Cell Stem Cell, 2019, 24(4):654-669
Clin Cancer Res, 2018, 24(11):2678-2687
Biochem Pharmacol, 2014, 89(1):52-61
S2475 Imatinib (STI571) Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Cell Host Microbe, 2021, 29(6):941-958.e10
Nat Commun, 2021, 12(1):51
Clin Cancer Res, 2021, 27(9):2533-2548
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cancer Res, 2021, canres.1222.2021
Cancers (Basel), 2021, 13(14)3635
Radiother Oncol, 2021, 157:175-181
S4001 Cabozantinib malate (XL184) Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(14)3635
S4947New Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Int J Mol Sci, 2021, 22(21)11770
S5077 Regorafenib (BAY-734506) Monohydrate Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Neoplasia, 2021, 23(3):304-325
S5240 Lenvatinib (E7080) Mesylate Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.
J Immunother Cancer, 2021, 9(6)e002305
Cancer Lett, 2021, 519:46-62
Cancers (Basel), 2021, 13(11)2539
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Front Oncol, 2021, 11:739139
Biochem Biophys Res Commun, 2021, 586:177-184
Cells, 2020, 9(6):E1452
S6662 AST-487 (NVP-AST487) AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.
Nat Commun, 2020, 21;11(1):1924
S7003 AZD2932 AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
Cancer Res, 2020, canres.1992.2020
Molecules, 2020, 8;25(9) pii: E2220
Development, 2016, 143(23):4394-4404
S7688 Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258, CHIR258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S7781 Sunitinib (SU11248) Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Adv Sci (Weinh), 2021, e2100881
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Blood Cancer J, 2021, 11(3):57
S7782 Dasatinib Monohydrate Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Nat Commun, 2021, 12(1):3705
Nucleic Acids Res, 2021, gkab538
S7818 Pexidartinib (PLX3397) Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.
Cell Death Dis, 2022, 13(1):33
Sci Transl Med, 2021, 13(598)eabd4550
J Exp Med, 2021, 218(8)e20210542
S8015 Agerafenib (RXDX-105) Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Mol Pharmacol, 2021, 99(6):435-447
Dis Model Mech, 2020, dmm.047779
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
J Cardiovasc Dev Dis, 2021, 8(3)28
Mol Med Rep, 2021, 23(4):1
CellPress, 2021, None
S8401 Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
Oncoimmunology, 2022, 11(1):2021619
Nature, 2021, 10.1038/s41586-020-03085-8
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
S8553 Avapritinib (BLU-285) Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
JCI Insight, 2020, 143474
J Pers Med, 2020, 10(4)E234
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
S8721 PDGFR inhibitor 1 PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.
S8757 Ripretinib (DCC-2618) DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.
Cancers (Basel), 2021, 13(15)3699
J Pers Med, 2020, 10(4)E234
Expert Opin Pharmacother, 2019, 20(13):1539-1550
S8780 AZD3229 AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
Front Immunol, 2020, 11:564133
Cell Signal, 2014, 26(1):149-61
S4947New Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Int J Mol Sci, 2021, 22(21)11770
Tags: c-Kit mutation | c-Kit receptor | c-Kit expression | c-Kit cancer | c-Kit signaling | c-Kit mutation analysis | c-Kit tyrosine kinase receptor | c-Kit proto-oncogene | c-Kit activation | c-Kit phosphorylation | c-Kit kinase activity | c-Kit inhibitor review